OSI-027 is an orally bioavailable mammalian inhibitor of mTOR kinase and has antineoplastic activity. OSI-027 binds to and inhibits of the catalytic site of mTOR, which is a central part of two protein complexes, mTORC1 and mTORC2, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. OSI-027 is in phase I clinical trial for the investigation on patients with advanced solid tumors or lymphoma.

Mequitamium iodide (LG 30435) is a quaternary ammonium phenothiazine. Mequitamium iodide was found to bind with high affinity only to histamine H1 receptors and to muscarinic acetylcholine receptors. The (+)-(S)-enantiomer is 10-fold more potent than (-)-(R)-enantiomer as a histamine antagonist, while the two enantiomers show the same antimuscarinic activity in vitro. In animal models, it exerts antiasthmatic and antiallergic properties. It was being clinically investigated as a treatment of asthma and rhinitis.

CT-2584 is a cytotoxic agent which modulates intracellular metabolism of phosphatidic acid in tumor cells. CT-2884 inhibits CTP:choline-phosphate cytidylyltransferase and causes de novo phospholipid biosynthesis via phosphatidic acid to be shunted away from phosphatidylcholine and into phosphatidylinositol. CT-2884 induced cytotoxicity is associated with disruption and swelling of endoplasmic reticulum and mitochondria. In the early 2000s, CT-2584 was investigated in phase 2 clinical trials for the treatment of prostate cancer and soft-tissue sarcoma. No development of the drug was reported since.

Cindunistat hydrochloride maleate (SD-6010) is an orally-administered, selective, time-dependent and irreversible inhibitor of human iNOS (hiNOS). In vivo studies using the canine anterior cruciate ligament-transection model have demonstrated that cindunistat improves synovial fluid nitrite and nitrotyrosine biomarkers, osteophyte formation and cartilage lesions. Cindunistat has also been shown to improve pain behaviour in rodent models of inflammatory and neuropathic pain. Based on its potential to inhibit NO production and an early clinical development programme, the disease-modifying efficacy and safety profile of cindunistat was studied in a 2-year proof-of-concept clinical trial of patients with knee OA. Cindunistat (50 or 200 mg/day) did not slow the rate of joint space narrowing versus placebo. After 48-weeks, KLG2 patients showed less joint space narrowing; however, the improvement was not sustained at 96-weeks. iNOS inhibition did not slow OA progression in KLG3 patients.

Glyphosate-isopropylammonium has herbicidal activity. Glyphosate-resistant (GR) soybeans have been developed so that products containing Glyphosate-isopropylammonium can be used as herbicides without harming the plant. Glyphosate-isopropylammonium is used in products such as Accord, Glyphomax and Durango. Because they contain the herbicide glyphosate, these products have been associated with a risk of developing cancer.

5-((4-(6-Chlorothieno[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile monofumarate (PRX-08066) is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist that causes selective vasodilation of pulmonary arteries. This drug was discovered and developed by Predix (later Epix) Pharmaceuticals and is being researched for the treatment of pulmonary arterial hypertension. In animal studies, PRX-08066 has been found to reduce several key indicators of pulmonary arterial hypertension and improved cardiac output, with similar efficacy to established drugs for this condition such as bosentan, sildenafil, beraprost and iloprost.

Resolvin E1 (RvE1 or RX-10001) is a trihydroxy eicosapentaenoic acid metabolite that has a role as an anti-inflammatory agent and a human xenobiotic metabolite. This compound binds to leukotriene B4 (BLT-1) on neutrophils and to ERV-1/ChemR23 on monocyte/macrophages. Resolvin E1 has been shown to reverse experimental periodontitis and dysbiosis in rats. Furthermore, in a murine model of Alzheimer’s disease, Resolvin E1 (in combination with lipoxin A4) decreased neuroinflammation. Resolvin E1 was also suggested as a potential therapeutic target for psoriasis. A phase I clinical trial to test drug safety in healthy volunteers has been completed in 2009.